NCT01276600

Dose-Proportionality and Intra-Individual Variability of Intracellular TFV-DP and FTC-TP in Healthy Volunteers

Dose-Proportionality and Intra-Individual Variability of Intracellular Tenofovir Diphosphate and Emtricitabine Triphosphate In Healthy Volunteers

• Status: Completed
• Phase: Phase 1
• Study type: Interventional
• Enrollment: 32 (actual)
• Sponsor: HIV Prevention Trials Network · Network
• Sex: All
• Age: 18 Years – 44 Years
• Healthy volunteers: Accepted

Summary

Describe the dose-proportionality and intra-individual variability of tenofovir diphosphate (TFV-DP) and emtricitabine triphosphate (FTC-TP) at steady-state in healthy human participants taking Truvada® (FTC 200mg/TDF 300 mg) under direct observation.

Detailed description

This PK study is designed to establish the dose-proportionality of TFV and FTC (serum and intracellular forms) with daily to weekly dosing. This information is essential to (1) employ drug concentration as an adherence measure in future PrEP studies, and (2) to estimate the anticipated concentration of parent and active moieties of TFV and FTC in intermittent PrEP regimens associated with full adherence to a prescribed regimen. In addition, intra-individual variability will be assessed to improve sample size estimates in future PrEP studies that use drug concentration as an adherence measure or where PK-PD correlations are planned. The dose-proportionality of intra-cellular phosphates of the two components of the study product has not previously been established. Given the complexity of movement of these drugs between body compartments (central compartment, vaginal mucosal tissue, vaginal lumen, gastrointestinal mucosal tissue, gastrointestinal lumen), into cells within these compartments, and intra-cellular phosphorylation, it is possible that non-dose proportional kinetics, such as mixed or zero-order saturable processes may be operating.

Conditions

• HIV

Interventions

Type	Name	Description
DRUG	Emtricitabine/tenofovir	200mg of emtricitabine 300mg of tenofovir

Timeline

• Start date: 2011-01-01
• Primary completion: 2011-10-01
• Completion: 2011-10-01
• First posted: 2011-01-13
• Last updated: 2025-03-25

Locations

2 sites across 1 country: United States